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Assay Detail

CHEMBL4367882

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.
Ghonim AE, Ligresti A, Rabbito A, Mahmoud AM, Di Marzo V, Osman NA, Abadi AH.
Eur J Med Chem (2019) 180 : 154 -170
PubMed 31302448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 6.88 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381791 1 7.39
CHEMBL4451793 1 6.36
CHEMBL4450238 1 -
CHEMBL4533663 1 -
CHEMBL4451217 1 -
CHEMBL4445661 1 -
CHEMBL4446746 1 -
CHEMBL4450401 1 -
CHEMBL4443713 1 -
CHEMBL4587737 1 -
CHEMBL4459664 1 -
CHEMBL4461356 1 -
CHEMBL4456654 1 -
CHEMBL4579868 1 -
CHEMBL4441442 1 -
CHEMBL4592199 1 -
CHEMBL4576974 1 -
CHEMBL4559193 1 -
CHEMBL4437741 1 -
CHEMBL4544293 1 -
CHEMBL4519212 1 -
CHEMBL4462864 1 -
CHEMBL4483617 1 -
CHEMBL4556046 1 -
CHEMBL4450995 1 -
CHEMBL4550200 1 -
CHEMBL4556423 1 -
CHEMBL3596703 1 -
CHEMBL4470152 1 -
CHEMBL1385951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381791 EC50 = 41.0 nM 7.39
CHEMBL4451793 EC50 = 436.5 nM 6.36
CHEMBL4579868 EC50 > 30000.0 nM -
CHEMBL4473769 EC50 > 30000.0 nM -
CHEMBL4456654 EC50 > 30000.0 nM -
CHEMBL4461356 EC50 > 30000.0 nM -
CHEMBL4459664 EC50 > 30000.0 nM -
CHEMBL4587737 EC50 > 30000.0 nM -
CHEMBL4443713 EC50 > 30000.0 nM -
CHEMBL4450401 EC50 > 30000.0 nM -
CHEMBL4446746 EC50 > 30000.0 nM -
CHEMBL4445661 EC50 > 30000.0 nM -
CHEMBL4451217 EC50 > 30000.0 nM -
CHEMBL4533663 EC50 > 30000.0 nM -
CHEMBL4450238 EC50 > 30000.0 nM -
CHEMBL4515942 EC50 > 30000.0 nM -
CHEMBL4468254 EC50 > 30000.0 nM -
CHEMBL4441442 EC50 > 30000.0 nM -
CHEMBL4592199 EC50 > 30000.0 nM -
CHEMBL4576974 EC50 > 30000.0 nM -
CHEMBL4559193 EC50 > 30000.0 nM -
CHEMBL4437741 EC50 > 30000.0 nM -
CHEMBL4544293 EC50 > 30000.0 nM -
CHEMBL4519212 EC50 > 30000.0 nM -
CHEMBL4462864 EC50 > 30000.0 nM -
CHEMBL4483617 EC50 > 30000.0 nM -
CHEMBL4556046 EC50 > 30000.0 nM -
CHEMBL4450995 EC50 > 30000.0 nM -
CHEMBL4550200 EC50 > 30000.0 nM -
CHEMBL4556423 EC50 > 30000.0 nM -
CHEMBL3596703 EC50 > 30000.0 nM -
CHEMBL4470152 EC50 > 30000.0 nM -
CHEMBL1385951 EC50 > 30000.0 nM -